title: Antiprotozoal activity of chloroquinoline based chalcones.
abstract: A new series of chloroquinoline based chalcones were synthesized and evaluated for in vitro antiamoebic and antimalarial activities. The results showed that out of fifteen compounds, four were found to be more active against the Entamoeba histolytica; while one compound was moderatively active compared to the standard drug metronidazole (IC50=1.46 μM). In contrast, in vitro antimalarial activity against the chloroquine-sensitive (3D7) strain of P. falciparum indicated relatively low activity when compared to controls such as chloroquine and quinine (IC50=0.0065 μM and 0.14 μM, respectively). The toxicological studies of these compounds on human breast cancer MCF-7 cell line showed that all the compounds were non-toxic at the concentration range of 1.56-50 μM.
authors.affiliation: Department of Chemistry, Jamia Millia Islamia, Jamia Nagar, New Delhi 110025, India.
authors.forename: Faisal
authors.initials: F
authors.lastname: Hayat
authors.forename: Emma
authors.initials: E
authors.lastname: Moseley
authors.forename: Attar
authors.initials: A
authors.lastname: Salahuddin
authors.forename: Robyn L
authors.initials: RL
authors.lastname: Van Zyl
authors.forename: Amir
authors.initials: A
authors.lastname: Azam
mesh_terms: D000981:Antiprotozoal Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D047188:Chalcones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D004354:Drug Screening Assays, Antitumor; D004748:Entamoeba histolytica / Q000187:drug effects*; D006801:Humans; D015394:Molecular Structure; D021261:Parasitic Sensitivity Tests; D010963:Plasmodium falciparum / Q000187:drug effects*; D011804:Quinolines / Q000737:chemistry*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D000981:Antiprotozoal Agents; D047188:Chalcones; D011804:Quinolines; C083774:2-chloroquinoline